MK-0457, an Aurora kinase and BCR-ABL inhibitor, is active in patients with BCR-ABL T315I leukemia.


Journal Article

MK-0457, an Aurora kinase and BCR-ABL inhibitor, was studied on a Phase I/II study in 77 patients with refractory hematologic malignancies. The average number of cycles per patient was 3 (range 1-21). Maximum tolerated doses for a 5-day short infusion and continuous infusion regimens were 40 mg/m(2)/h and 144 mg/m(2)/h, respectively. Drug-related adverse events (AEs) included transient mucositis and alopecia. Eight of 18 patients with BCR-ABL T315I-mutated chronic myelogenous leukemia (44%) had hematologic responses and one of three patients (33%) with Philadelphia chromosome-positive acute lymphoblastic leukemia obtained complete remission. MK-0457 has important activity in patients with leukemias expressing the highly resistant T315I BCR-ABL mutation.

Full Text

Duke Authors

Cited Authors

  • Giles, FJ; Swords, RT; Nagler, A; Hochhaus, A; Ottmann, OG; Rizzieri, DA; Talpaz, M; Clark, J; Watson, P; Xiao, A; Zhao, B; Bergstrom, D; Le Coutre, PD; Freedman, SJ; Cortes, JE

Published Date

  • January 2013

Published In

Volume / Issue

  • 27 / 1

Start / End Page

  • 113 - 117

PubMed ID

  • 22772060

Pubmed Central ID

  • 22772060

Electronic International Standard Serial Number (EISSN)

  • 1476-5551

Digital Object Identifier (DOI)

  • 10.1038/leu.2012.186


  • eng

Conference Location

  • England